Design, Synthesis and Pharmacological Evaluation of Novel 4-Phenoxyquinoline Derivatives as Potential Antitumor Agents

作者：Hu Hao; Jiang Mingyan; Xie Lijun; Hu Gang; Zhang Cuirong; Zhang Lixia; Zhou Shunguang; Zhang Meihui^*; Gong Ping

来源：Chemical Research in Chinese Universities, 2015, 31(5): 746-755.

DOI：10.1007/s40242-015-5166-3

• 4-Phenoxyquinoline derivative
• Cytotoxic activity
• 3-Amino-2-cyano-acrylamide

A series of novel 4-phenoxyquinoline derivatives containing 3-amino-2-cyano-acrylamide framework was designed and synthesized, and the in vitro cytotoxic activities of them against five cancer cell lines(HT-29, H460, A549, MKN-45, and U87MG) were evaluated. Most of the compounds exhibited moderate-to-significant cytotoxicity and high selectivity against one or more cell lines as compared with Foretinib. The studies of their preliminary structure-activity relationships(SARs) indicate that the compounds containing methyl groups, especially methyl groups at 4-position of the phenyl ring(moiety B) are more effective. Among them, compound 36 shows the most potent antitumor activities with IC50 values of 0.04, 0.09, 0.67, 0.39 and 1.10 mu mol/L against HT-29, H460, A549, MKN-45 and U87MG cell lines, respectively.

• 出版日期2015-10
• 单位沈阳药科大学; 福建省微生物研究所